# US 10,245,331 B2 · Cromolyn derivatives and related methods of imaging and treatment

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- Number: US 10,245,331 B2
- Document ID: US10245331B2
- Status: Granted
- Kind: B2
- Application number: 15/899,644
- Filed: 2018-02-20
- Published: 2018-06-21
- Granted: 2019-04-02
- Earliest claimed: 2009-01-29
- Assignees: The General Hospital Corporation
- Applicants: The General Hospital Corporation
- Inventors: David R. Elmaleh
- Web page: https://patentgrep.com/patent/US10245331B2

## CPC

- A61K 51/0421: {having six-membered rings with one oxygen as the only ring hetero atom}
- A61P 25/28: for treating neurodegenerative disorders of the central nervous system, e.g. nootropic agents, cognition enhancers, drugs for treating Alzheimer's disease or other forms of dementia
- C07D 311/24: with carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, e.g. ester or nitrile radicals, directly attached in position 2
- A61K: PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES (devices or methods specially adapted for bringing pharmaceutical products into particular physical or administering forms A61J3/00; chemical aspects of, or use of materials for deodorisation of air, for disinfection or sterilisation, or for bandages, dressings, absorbent pads or surgical articles A61L; soap compositions C11D)
- A61P: SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- C07D: HETEROCYCLIC COMPOUNDS (macromolecular compounds C08)

## Abstract

Novel cromolyn analogs useful as imaging agents for detecting atherosclerotic plaques and for treating atherosclerosis and Alzheimer's Disease, and methods of making the cromolyn analogs, are disclosed. The cromolyn analogs have the general formula: wherein: X is OH, C1-C6 alkoxyl; Y and Z are independently selected form a C1-C6 alkyl, C1-C6 alkoxyl, halogen, un-substituted or C1-C6 substituted amine, 18F, 19F, or H; and n is 1, 2, or 3; and wherein for structure (I), if n are both 1 and Y and Z are both H and X is OH.

## Claims

### Claim 1

A method for treating Alzheimer's disease in a subject in need thereof consisting of co-administering:
by inhalation cromolyn sodium in the form of a dry powder, and
by mouth from 1 mg to 25 mg of ibuprofen per day,
wherein the dry powder is micronized and further comprises an excipient.

### Claim 2 (depends on 1)

The method of claim 1, wherein 1 mg, 2 mg, 5 mg, 10 mg, or 25 mg of ibuprofen per day are co-administered.

### Claim 3 (depends on 1)

The method of claim 1, wherein 1 mg, 2 mg, 5 mg, or 10 mg of ibuprofen per day are co-administered.

### Claim 4 (depends on 1)

The method of claim 1, wherein 10 mg or 25 mg of ibuprofen per day are co-administered.

### Claim 5 (depends on 1)

The method of claim 1, wherein the excipient is lactose monohydrate.

### Claim 6 (depends on 1)

The method of claim 1, wherein 0.05 to 0.5 mg/kg per day of cromolyn sodium are administered.

### Claim 7 (depends on 1)

The method of claim 1, wherein the dry powder further comprises a pharmaceutically acceptable carrier.

### Claim 8

A method for treating Alzheimer's disease in a subject in need thereof consisting of co-administering:
by inhalation cromolyn sodium in the form of a dry powder, and
by mouth 10 mg of ibuprofen per day,
wherein the dry powder is micronized and further comprises an excipient.

### Claim 9 (depends on 8)

The method of claim 8, wherein the excipient is lactose monohydrate.

### Claim 10 (depends on 8)

The method of claim 8, wherein 0.05 to 0.5 mg/kg per day of cromolyn sodium are administered.

### Claim 11 (depends on 8)

The method of claim 8, wherein the dry powder further comprises a pharmaceutically acceptable carrier.